2 - phenyl - m - ditianderivat to anvendning as intermediate products for the synthesis of m - ditianderivat with koronardilaterande characteristics

摘要

1489088 Aminoketones F HOFFMANN-LA ROCHE & CO AG 20 Dec 1974 [21 Dec 1973] 23143/77 Divided out of 1489086 Heading C2C The invention comprises novel compounds (I) wherein R represents a group of the Formula (Ia) or (Ib) in which R 1 , R 2 and R 3 each represent a hydrogen or halogen atom or a lower alkyl, lower alkoxy, aryl-(lower alkoxy), aryloxy, phenyl, nitro, amino, lower alkylthio, trifluoromethyl, hydroxy, cyano, di(lower alkyl)amino, lower alkanoylamino, carboxyl, lower alkoxycarbonyl, lower alkylsulphonyl, hydroxymethyl, lower alkanoyloxy, amido, lower alkanoyl, sulphamoyl, mono(lower alkyl) sulphamoyl, di(lower alkyl) sulphamoyl, aminocarbonyloxy, mono(lower alkyl) aminocarbonyloxy or (lower alkylamino)-(lower alkyl) group or two adjacent R 1 , R 2 and R 3 symbols together represent a methylenedioxy, ethylenedioxy or butadien- 1,3-ylene-1,4 group, R 4 represents a hydrogen atom or a lower alkyl group, R 5 , R 6 and R 7 each represent a hydrogen or halogen atom or a lower alkyl, lower alkoxy, hydroxy or benzyloxy group or two adjacent R 5 , R 6 and R 7 symbols together represent a methylenedioxy or ethylenedioxy group, Y represents a straight-chain or branched-chain, optionally hydroxy-substituted, aliphatic group containing 2-8 carbon atoms, of which 2-4 carbon atoms are present in the chain, and Z represents a straight-chain or branched-chain, optionally hydroxy-substituted aliphatic group containing 1-8 carbon atoms, of which 1-4 carbon atoms are present in the chain, and m stands for zero or 1, or an acid addition salt thereof; the groups qualified by lower contain up to 6 carbons and aryl signifies phenyl optionally substituted by halogen, lower alkyl, lower alkoxy, NO 2 and amino. The compounds are made by acylating appropriate amines utilizing RCOY.Cl. 3,4 - Dimethoxy - - chlorobutyrophenone is made by condensing veratrol and 4-chlorobutyric acid in the presence of polyphosphoric acid.